首页|Micelle morphology phase diagram in a phospholipid, PEGylated lipid, and peptide amphiphiles ternary system
Micelle morphology phase diagram in a phospholipid, PEGylated lipid, and peptide amphiphiles ternary system
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Conjugating peptides with alkyl tails and/or polymer chains to form peptide amphiphiles (PAs) allows self-assembly of PA together with other amphiphilic molecules to nanos-tructures for better peptide stability, longer blood circulation time, and facilitated cell uptake. The morphological transformation of the nanostructures significantly affects the pharmacokinetics and efficacy of the bioactive peptide. We report here the systematical study of the micelle morphological transformation in a ternary system consisting of a phospholipid, a PEGylated lipid, and a model PA (Myr-M3mP6, formed by attaching the novel anti-platelet peptide M3mP6 with the myristoyl group). The size and morphology of the self-assembled nanostructures were characterized by using dynamic light scattering and liquid cell - scanning transmission electron microscopy (LC-STEM). The morphologies of the self-assembled structures are mapped to a phase diagram with three coordinates denoted as the molar percentages of the PEGylated lipid, phospholipid, and Myr-M3mP6. The results provide a guidance for PA lipid formulation design and optimization. In addition, the effect of mixing kinetics is evaluated and a scalable process is developed for the potential of continuous, mass production of the stable micelles with the targeted morphology, size, and peptide loading.
Drug deliverySelf-assemblyMorphological transformationLipopeptideLiquid cell electron microscopy imagingDynamic light scattering
Chang Liu、Sherry Gong、Xiaoping Du
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Department of Chemical Engineering, University of Illinois Chicago, Chicago, IL 60607, USA
Department of Pharmacology and Regenerative Medicine, University of Illinois Chicago, Chicago, IL 60607, USA
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